Development and Optimization of Glaser–Hay Bioconjugations

The prevalence of bioconjugates in the biomedical sciences necessitates the development of novel mechanisms to facilitate their preparation. Towards this end, the translation of the Glaser–Hay coupling to an aqueous environment is examined, and its potential as a bioorthogonal conjugation reaction is demonstrated. This optimized, novel, and aqueous Glaser–Hay reaction is applied towards the development of bioconjugates utilizing protein expressed with an alkynyl unnatural amino acid. Unnatural amino acid technology provides a degree of bioorthognality and specificity not feasible with other methods. Moreover, the scope of the reaction is demonstrated through protein–small molecule couplings, small‐molecule–solid‐support couplings, and protein–solid‐support immobilizations.     

Alternative Synthesis and Structures of C‐monoacetylenic Phosphaalkenes

An alternative synthesis of C‐monoacetylenic phosphaalkenes trans‐Mes*P=C(Me)(C≡CR) (Mes* = 2, 4, 6‐^tBu₃Ph, R = Ph, SiMe₃) from C‐bromophosphaalkenes cis‐Mes*P=C(Me)Br using standard Sonogashira coupling conditions is described. Crystallographic studies confirm cis‐trans isomerization of the P=C double bond during Pd‐catalyzed cross coupling, leading exclusively to trans‐acetylenic phosphaalkenes. Crystallographic studies of all synthesized compounds reveal the extend of π‐conjugation over the acetylene and P=C π‐systems.     

A Study of the Constituents of the Heartwood of Tsuga Chinensis Pritz. Var. Formosana (Hay.)

By means of spectroscopic analysis, X-ray crystallography and chemical correlation the heartwood of Taiwan hemlock was found to contain compounds of sterols, carboxylic acids, 13-epimanool, o methoxyphenolics, coniferaldehyde, benzofuranoid neolignan, α-conidendrin, tsugacetal, isolariciresinol, secoisolariciresinol, matairesinol, hydroxymatairesinol and oxomatairesinol. Among them (+)-tsugacetal is a novel lignan acetal having an α-conidendrin related structure with the acetal methoxy group at the β-position.     

茴藿香精油化学成分的研究

本文介绍采用毛细管气相色谱-质谱法研究了甘肃敦煌栽培的茴霍香精油的化学成分。色谱分离出30多个组分,质谱鉴定了25种化合物,占色谱流出峰总面积的97.87%。其中有19种化合物为该植物化学成分的首次报道。异薄荷酮(35.22)、茴香脑(24.30%)和长叶薄荷酮(16.66%)为该精油的主要成分。     

发现于温州的浙江植物区系新资料

报道了发现于温州的2个浙江植物分布新记录属和4个新记录种,2个新记录属分别是吻兰属(Collabium Bl.)和刺蕊草属(Pogostemon Desf.),4个新记录种分别是台湾吻兰(Collabium formosanum Hayata)、翘距虾脊兰(Calanthe aristulifera Rchb. f.)、水珍珠菜(Pogostemon auricularius (Linn.) Kassk.)和疏花车前(Plantago asiatica Linn. subsp. erosa (Wall.) Z Y LI).凭证标本保存于温州大学标本馆(WZU).     

Two isomeric epoxysitosterols from Rhododendron formosanum: 1H and 13C NMR chemical shift assignments

1H and 13C NMR assignments of the two isomeric epoxysitosterols, 5,6 alpha-epoxy-5 alpha-stigmastan-3 beta-ol (1) and 5,6 beta-epoxy-5 beta-stigmastan-3 beta-ol (2), isolated from the leaves of Rhododendron formosanum Hemsl were achieved by 1D and 2D techniques such as DEPT, HMBC, HMQC, COSY and NOESY.     

Djulis (Chenopodium formosanum) and Its Bioactive Compounds Protect Human Lung Epithelial A549 Cells from Oxidative Injury Induced by Particulate Matter via Nrf2 Signaling Pathway

The protective effects of water extracts of djulis (Chenopodium formosanum) (WECF) and their bioactive compounds on particulate matter (PM)-induced oxidative injury in A549 cells via the nuclear factor-erythroid 2-related factor 2 (Nrf2) signaling were investigated. WECF at 50–300 µg/mL protected A549 cells from PM-induced cytotoxicity. The cytoprotection of WECF was associated with decreases in reactive oxygen species (ROS) generation, thiobarbituric acid reactive substances (TBARS) formation, and increases in superoxide dismutase (SOD) activity and glutathione (GSH) contents. WECF increased Nrf2 and heme oxygenase-1 (HO-1) expression in A549 cells exposed to PM. SP600125 (a JNK inhibitor) and U0126 (an ERK inhibitor) attenuated the WECF-induced Nrf2 and HO-1 expression. According to the HPLC-MS/MS analysis, rutin (2219.7 µg/g) and quercetin derivatives (2648.2 µg/g) were the most abundant bioactive compounds present in WECF. Rutin and quercetin ameliorated PM-induced oxidative stress in the cells. Collectively, the bioactive compounds present in WECF can protect A549 cells from PM-induced oxidative injury by upregulating Nrf2 and HO-1 via activation of the ERK and JUN signaling pathways.     

Fast and non–derivative method based on high–performance liquid chromatography–charged aerosol detection for the determination of fatty acids from Agastache rugosa (Fisch. et Mey.) O. Ktze. seeds

This study utilised response surface methodology to optimise the conditions for the extraction of A. rugosa seeds oil (ARO). Single–factor experiment and response surface methodology (RSM) were performed to identify the extraction time, liquid–solid ratio and extraction temperature that provided the highest yield of ARO. The optimal extraction time, liquid–solid ratio and extraction temperature were 8 h, 4:1 mL/g and 55 °C. The fatty acids (FAs) content and oil yield obtained through the optimised impregnation–extraction process were 19.67 mg/g and 32.1%. These values matched well with the predicted values. Linolenic acid was identified to be the main active ingredient of ARO. The high–performance liquid chromatography–charged aerosol detection method presented here is fast and does not require derivatisation. Therefore, it could be used to quantitatively analyse the FAs present in ARO and applied to detect compounds with low or no ultraviolet response.     

火焰原子吸收法测定藿香中的微量元素

采用火焰原子吸收法测定了广藿香与土藿香中Ca、Mn、Fe、K、Cu、Mg、Zn七种微量元素的含量.方法的回收率在95.6%～110.0%之间,RSD在0.9%～2.5%之间,具有良好的准确度和精密度.结果表明,广藿香中Mn、Fe、K、Cu、Zn等五种元素的含量较为丰富,特别是Mn、K两种元素的含量远高于土藿香.此测定结果可作为探讨藿香中微量元素的含量与药效相关性的科学依据.